Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase

Journal of Medicinal Chemistry

Volumn 54, Issue 20, 2011, Pages 7150-7164

  Wang, Lei ^a   Desmoulin, Sita Kugel ^c   Cherian, Christina ^b   Polin, Lisa ^b,c   White, Kathryn ^b,c   Kushner, Juiwanna ^b,c   Fulterer, Andreas ^d   Chang, Min Hwang ^d   Mitchell Ryan, Shermaine ^c   Stout, Mark ^e   Romero, Michael F ^d   Hou, Zhanjun ^b,c   Matherly, Larry H ^b,c   Gangjee, Aleem ^a  

^a DUQUESNE UNIVERSITY   (United States)

^b KARMANOS CANCER INSTITUTE   (United States)

^c WAYNE STATE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^d MAYO GRADUATE SCHOOL   (United States)

^e CHILDREN'S HOSPITAL OF MICHIGAN   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA GLYCINAMIDE RIBONUCLEOTIDE FORMYLTRANSFERASE; FOLATE RECEPTOR; FOLIC ACID ANTAGONIST; LOMETREXOL; METHOTREXATE; PEMETREXED; PHOSPHORIBOSYLGLYCINAMIDE FORMYLTRANSFERASE; PROTON COUPLED FOLATE TRANSPORTER; PYRROLO [2,3 D] PYRIMIDINE; RALTITREXED; REDUCED FOLATE CARRIER; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CELL PROLIFERATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN CELL; MEMBRANE TRANSPORT; MOUSE; NONHUMAN; TUMOR CELL;

ADENOSINE TRIPHOSPHATE; ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; FOLATE RECEPTOR 1; FOLATE RECEPTOR 2; FOLIC ACID ANTAGONISTS; GLUTAMATES; HUMANS; MICE; MICE, SCID; NEOPLASM TRANSPLANTATION; OOCYTES; PATCH-CLAMP TECHNIQUES; PHOSPHORIBOSYLGLYCINAMIDE FORMYLTRANSFERASE; PROTON-COUPLED FOLATE TRANSPORTER; PYRIMIDINES; PYRIMIDINONES; REDUCED FOLATE CARRIER PROTEIN; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS; XENOPUS;

EID: 80054932788     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200739e     Document Type: Article

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